UA84399C2 - Process for the preparation of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl] ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazol-3-one - Google Patents

Process for the preparation of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl] ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazol-3-one

Info

Publication number
UA84399C2
UA84399C2 UA20041109407A UA20041109407A UA84399C2 UA 84399 C2 UA84399 C2 UA 84399C2 UA 20041109407 A UA20041109407 A UA 20041109407A UA 20041109407 A UA20041109407 A UA 20041109407A UA 84399 C2 UA84399 C2 UA 84399C2
Authority
UA
Ukraine
Prior art keywords
triazol
morpholinyl
fluorophenyl
dihydro
trifluoromethyl
Prior art date
Application number
UA20041109407A
Other languages
Russian (ru)
Inventor
Марк Хаффман
Махмуд С. Каба
Джозеф Ф. Пейак
Девид Хендз
Original Assignee
Мерк Энд Ко., Инк.
Мерк Шарп Енд Доме Лимитед
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Мерк Энд Ко., Инк., Мерк Шарп Енд Доме Лимитед filed Critical Мерк Энд Ко., Инк.
Publication of UA84399C2 publication Critical patent/UA84399C2/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms

Abstract

The present invention is concerned with a novel process for the preparation of the compound 5-[[2(R)-[l(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)4-morpholinyl]methyl]-l,2-dihydro-3H-l,2,4-triazol-3-one. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of psychiatric disorders, inflammatory diseases and emesis.
UA20041109407A 2002-04-18 2003-04-17 Process for the preparation of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl] ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazol-3-one UA84399C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37373402P 2002-04-18 2002-04-18
PCT/US2003/011956 WO2003089429A1 (en) 2002-04-18 2003-04-17 Process for 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazol-3-one

Publications (1)

Publication Number Publication Date
UA84399C2 true UA84399C2 (en) 2008-10-27

Family

ID=29251070

Family Applications (1)

Application Number Title Priority Date Filing Date
UA20041109407A UA84399C2 (en) 2002-04-18 2003-04-17 Process for the preparation of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl] ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazol-3-one

Country Status (21)

Country Link
US (1) US7847095B2 (en)
EP (1) EP1499611B1 (en)
JP (1) JP4271586B2 (en)
KR (1) KR100982901B1 (en)
CN (1) CN1293077C (en)
AR (1) AR039625A1 (en)
AU (1) AU2003228578B2 (en)
BR (1) BR0309277A (en)
CA (1) CA2482466C (en)
EG (1) EG24127A (en)
HR (1) HRP20040974A2 (en)
IL (1) IL164586A (en)
MX (1) MXPA04010182A (en)
NO (1) NO330362B1 (en)
NZ (1) NZ535883A (en)
PL (1) PL217076B1 (en)
RU (1) RU2326879C2 (en)
TW (1) TWI341313B (en)
UA (1) UA84399C2 (en)
WO (1) WO2003089429A1 (en)
ZA (1) ZA200408193B (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0400850D0 (en) * 2004-03-30 2004-03-31 Astrazeneca Ab Novel Compounds
EP2266980A1 (en) 2005-10-05 2010-12-29 Ranbaxy Laboratories Limited Polymorphic form of aprepitant intermediate
EP1942734A4 (en) * 2005-10-06 2010-04-07 Reddys Lab Ltd Dr Preparation of aprepitant
US9227958B2 (en) 2006-02-03 2016-01-05 Glenmark Pharmaceuticals Limited Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
EP2057151A4 (en) * 2006-08-28 2010-07-21 Hetero Drugs Ltd Process for purification of aprepitant
US8940890B2 (en) 2010-05-24 2015-01-27 Chengdu Di'ao Pharmaceutical Group Co., Ltd. Preparation method of 5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one
HUP1000325A2 (en) * 2010-06-18 2012-01-30 Druggability Technologies Ip Holdco Jersey Ltd Nanostructured aprepitant compositions and process for their preparation
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
CN103030668B (en) * 2011-10-09 2016-06-15 江苏豪森药业集团有限公司 A kind of method preparing fosaprepitant
PT2817305T (en) * 2012-02-23 2016-11-02 Piramal Entpr Ltd An improved process for the preparation of aprepitant
CZ304770B6 (en) 2012-03-13 2014-10-08 Zentiva, K.S. Process for preparing 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorfenyl)morpholino)methyl)-1H-1,2,4-triazol-5(4H)-one (aprepitant) in polymorphous form II
ITMI20130273A1 (en) * 2013-02-26 2014-08-27 Olon Spa PROCEDURE FOR THE PREPARATION OF APREPITANT
CN103288813A (en) * 2013-06-04 2013-09-11 四川百利药业有限责任公司 Preparation method of aprepitant
CN107954998B (en) * 2016-10-14 2022-08-12 江苏豪森药业集团有限公司 Preparation method of fosaprepitant intermediate
CN106967057A (en) * 2017-06-01 2017-07-21 四川制药制剂有限公司 A kind of efficient preparation technology of Aprepitant

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5719147A (en) 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US5637699A (en) 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
IL111960A (en) * 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
GB9513972D0 (en) * 1995-07-08 1995-09-06 Merck Sharp & Dohme Pharmaceutical compositions
ZA985765B (en) * 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
GB9813025D0 (en) 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis

Also Published As

Publication number Publication date
NZ535883A (en) 2007-12-21
CA2482466C (en) 2012-11-20
NO20045001L (en) 2004-11-17
EP1499611A1 (en) 2005-01-26
EP1499611B1 (en) 2015-02-11
AR039625A1 (en) 2005-03-02
JP4271586B2 (en) 2009-06-03
US7847095B2 (en) 2010-12-07
IL164586A (en) 2010-11-30
HRP20040974A2 (en) 2005-06-30
MXPA04010182A (en) 2005-02-03
AU2003228578B2 (en) 2009-07-30
CN1293077C (en) 2007-01-03
JP2005529881A (en) 2005-10-06
TW200400189A (en) 2004-01-01
NO330362B1 (en) 2011-04-04
IL164586A0 (en) 2005-12-18
WO2003089429A1 (en) 2003-10-30
BR0309277A (en) 2005-02-22
CA2482466A1 (en) 2003-10-30
PL373348A1 (en) 2005-08-22
US20050215786A1 (en) 2005-09-29
KR20050007299A (en) 2005-01-17
KR100982901B1 (en) 2010-09-20
RU2326879C2 (en) 2008-06-20
ZA200408193B (en) 2006-06-28
CN1646525A (en) 2005-07-27
AU2003228578A1 (en) 2003-11-03
TWI341313B (en) 2011-05-01
EG24127A (en) 2008-07-08
PL217076B1 (en) 2014-06-30
RU2004133678A (en) 2005-05-27
EP1499611A4 (en) 2006-05-03

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